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NV-5440

Chemical Structure : NV-5440

CAS No.: 2226614-88-4

NV-5440 (NV5440)

Catalog No.: PC-20247Not For Human Use, Lab Use Only.

NV-5440 (NV5440) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 70 nM, directly targets GLUT-1 with Ki of 69.3 nM.

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    Biological Activity

    NV-5440 (NV5440) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 70 nM, directly targets GLUT-1 with Ki of 69.3 nM.
    NV-5440 shows no substantial off-target activity (>75% inhibition at 10 μM) in a panel of kinases.
    NV-5440 inhibits glucose uptake inhibition with IC50 of 36 and 140 nM in MCF7 and HUVECs, respectively.
    NV-5440 showspotent inhibition of glucose uptake by GLUT1 at 8 nM, shows significantly less inhibition of glucose uptake by both GLUT3 and GLUT4, with IC50 values of 270 and 390 nM, respectively.
    NV-5440 acts as a potent inhibitor of glycolysis at multiple points in the glycolysis pathway.

    Physicochemical Properties

    M.Wt 572.73
    Formula C31H36N6O3S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-[4-[5-[[4-(2-Cyanophenyl)-1-piperazinyl]methyl]-2,4-dimethylbenzoyl]-1-piperazinyl]-benzenesulfonamide

    References

    1. Kang SA, et al. Cell Chem Biol. 2019 Sep 19;26(9):1203-1213.e13.

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